Assay Detail
Binding
CHEMBL898343
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Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 8.17 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL236014 | — | — | 1 | 9.10 |
| CHEMBL235190 | — | — | 1 | 9.10 |
| CHEMBL393716 | — | — | 1 | 9.00 |
| CHEMBL236423 | — | — | 1 | 8.74 |
| CHEMBL236424 | — | — | 1 | 8.74 |
| CHEMBL236015 | — | — | 1 | 8.64 |
| CHEMBL237050 | — | — | 1 | 8.60 |
| CHEMBL236839 | — | — | 1 | 8.48 |
| CHEMBL237267 | — | — | 1 | 8.48 |
| CHEMBL236940 | — | — | 1 | 8.35 |
| CHEMBL236650 | — | — | 1 | 8.35 |
| CHEMBL237266 | — | — | 1 | 8.22 |
| CHEMBL391914 | — | — | 1 | 8.19 |
| CHEMBL237268 | — | — | 1 | 8.15 |
| CHEMBL391427 | — | — | 1 | 8.12 |
| CHEMBL236872 | — | — | 1 | 8.06 |
| CHEMBL236731 | — | — | 1 | 8.01 |
| CHEMBL236625 | — | — | 1 | 8.00 |
| CHEMBL439560 | — | — | 1 | 7.96 |
| CHEMBL236732 | — | — | 1 | 7.58 |
| CHEMBL236627 | — | — | 1 | 7.58 |
| CHEMBL391219 | — | — | 1 | 7.54 |
| CHEMBL237080 | — | — | 1 | 7.42 |
| CHEMBL393715 | — | — | 1 | 7.41 |
| CHEMBL236838 | — | — | 1 | 7.33 |
| CHEMBL237049 | — | — | 1 | 7.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL236014 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL235190 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL393716 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL236423 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL236424 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL236015 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL237050 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL236839 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL237267 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL236940 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL236650 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL237266 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL391914 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL237268 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL391427 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL236872 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL236731 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL236625 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL439560 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL236732 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL236627 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL391219 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL237080 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL393715 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL236838 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL237049 | — | Ki | = | 49.0 | nM | 7.31 |